Drug intelligence / Profile preview

cyclizine + dexamethasone

Development stage
Unknown
Lead developer
GSK
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Subcutaneous, Intravenous, Intramuscular, Oral
01

Overview

Cyclizine + dexamethasone is a combination of two pharmaceutical drugs used primarily for the prevention and management of nausea and vomiting, particularly in postoperative settings and palliative care. Cyclizine is a piperazine-derivative antihistamine with antiemetic, antivertigo, anticholinergic, and central nervous system depressant properties. It acts mainly by blocking histamine H1 receptors and exerting anticholinergic effects on the medullary chemoreceptor trigger zone to reduce nausea and vomiting[10][7]. Dexamethasone is a synthetic fluorinated glucocorticoid with potent anti-inflammatory and immunosuppressive actions; it reduces inflammation by binding to glucocorticoid receptors, modulating gene expression, suppressing pro-inflammatory cytokines, and stabilizing cell membranes[6][8]. The combination may be used when single-agent therapy is insufficient or as part of multimodal antiemetic regimens in perioperative or cancer care settings[1][7].

02

Targets

mAChR (Muscarinic acetylcholine receptors)GR (Glucocorticoid receptor)HRH1 (Histamine H1 Receptor)

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